Clissold S P
Drugs. 1986;32 Suppl 4:8-26. doi: 10.2165/00003495-198600324-00003.
After almost 90 years of clinical use, aspirin remains one of the world's most extensively used 'over-the-counter' drugs, and it is still recognised as the standard analgesic/antipyretic/anti-inflammatory agent by which newer drugs are assessed. However, its pre-eminent position as the analgesic of choice for mild to moderate pain has been seriously challenged with the introduction of many 'new' non-steroidal non-narcotic analgesic drugs. Indeed, there is convincing scientific evidence that many of the 'newer' non-steroidal drugs such as diflunisal, ibuprofen, flurbiprofen etc. are significantly superior analgesics and, in many cases, have a longer duration of action. In recent years the salicylates, aspirin in particular, have been the focus of much attention regarding their side effect profiles. At usual dosages for relief of pain and during occasional use, aspirin is well tolerated by the vast majority of patients. Adverse reactions, of which there is a wide spectrum, most frequently accompany anti-inflammatory doses of aspirin, or may be the result of accidental overdosing (particularly in children and the elderly)--probably a reflection of the lay population's acceptability of aspirin's presumed safety. As with other non-steroidal analgesic drugs, gastrointestinal complaints are the most commonly reported side effects. The existence of many shared clinical, adverse and toxic effects of aspirin and other non-steroidal anti-inflammatory drugs (NSAIDs) is thought to be accounted for by a common mechanism--inhibition of the ubiquitous cyclo-oxygenase enzyme. Thus, suppression of prostaglandin biosynthesis is widely considered to explain the common properties of NSAIDS, although further research is still necessary to clarify some inconsistencies and to complete our understanding of the processes involved. Aspirin and salicylates have been reported to have a wide range of drug interactions but only relatively few seem to be clinically important. Many of the interactions are pharmacokinetic in nature. Drugs considered to produce the most significant interactions with salicylates include anticoagulants and thrombolytic agents, uricosuric agents, corticosteroids, methotrexate and sulphonylurea hypoglycaemic agents.
在经过近90年的临床应用后，阿司匹林仍然是世界上使用最广泛的“非处方药”之一，并且它仍然被公认为评估新型药物的标准止痛/退热/抗炎药物。然而，随着许多“新型”非甾体非麻醉性止痛药物的推出，其作为轻至中度疼痛首选止痛药的卓越地位受到了严峻挑战。事实上，有令人信服的科学证据表明，许多“新型”非甾体药物，如双氟尼酸、布洛芬、氟比洛芬等，是明显更优的止痛药，而且在许多情况下，作用持续时间更长。近年来，水杨酸盐，尤其是阿司匹林，因其副作用情况而备受关注。在用于缓解疼痛的常规剂量下以及偶尔使用时，绝大多数患者对阿司匹林耐受性良好。不良反应种类繁多，最常伴随阿司匹林的抗炎剂量出现，或者可能是意外过量用药的结果（尤其是在儿童和老年人中）——这可能反映了普通民众对阿司匹林假定安全性的接受程度。与其他非甾体止痛药物一样，胃肠道不适是最常报告的副作用。阿司匹林和其他非甾体抗炎药（NSAIDs）存在许多共同的临床、不良和毒性作用，被认为是由一种共同机制——抑制普遍存在的环氧化酶所导致。因此，虽然仍需要进一步研究来澄清一些不一致之处并完善我们对相关过程的理解，但普遍认为前列腺素生物合成的抑制解释了NSAIDs的共同特性。据报道，阿司匹林和水杨酸盐有广泛的药物相互作用，但似乎只有相对较少的相互作用在临床上具有重要意义。许多相互作用本质上是药代动力学的。被认为与水杨酸盐产生最显著相互作用的药物包括抗凝剂和溶栓剂、促尿酸排泄剂、皮质类固醇、甲氨蝶呤和磺酰脲类降糖药。
